0000000000003996

AUTHOR

Octavio Díez-sales

showing 36 related works from this author

Sorbitol-penetration enhancer containing vesicles loaded with baicalin for the protection and regeneration of skin injured by oxidative stress and UV…

2018

Abstract Aiming at improving the protective effects of baicalin on the skin, new highly-biocompatible penetration enhancer containing vesicles (PEVs) were developed by modifying the base formulation of transfersomes with sorbitol, thus obtaining sorbitol-PEVs. An extensive evaluation of the physico-chemical features of both transfersomes and sorbitol-PEVs was carried out. Transfersomes were mainly close-packed, multi-compartment vesicles, while sorbitol-PEVs appeared mostly as single, spherical, unilamellar vesicles. All the vesicles were small in size (∼128 nm) and negatively charged (∼−67 mV), without significant differences between the formulations. The in vitro delivery of baicalin to i…

SwineUltraviolet RaysChemistry PharmaceuticalCellPharmaceutical Science02 engineering and technologymedicine.disease_cause030226 pharmacology & pharmacyCell LineExcipients03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineDrug Delivery SystemsCell MovementmedicineAnimalsHumansRegenerationSorbitolParticle SizeCell ProliferationSkinFlavonoidsWound HealingCell growthVesicleRegeneration (biology)fungi3T3 Cells021001 nanoscience & nanotechnologyIn vitroOxidative Stressmedicine.anatomical_structurechemistryBiophysicsSorbitol0210 nano-technologyBaicalinOxidative stressInternational journal of pharmaceutics
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Nutriosomes: Prebiotic delivery systems combining phospholipids, a soluble dextrin and curcumin to counteract intestinal oxidative stress and inflamm…

2018

Nutriosomes, new phospholipid nanovesicles specifically designed for intestinal protection were developed by simultaneously loading a water-soluble dextrin (Nutriose® FM06) and a natural antioxidant (curcumin). Nutriosomes were easily fabricated in a one-step, organic solvent-free procedure. The stability and delivery performances of the vesicles were improved by adding hydroxypropyl methylcellulose. All the vesicles were small in size (mean diameter ∼168 nm), negatively charged (zeta potential ∼-38 mV, irrespective of their composition), and self-assembled predominantly in unilamellar vesicles stabilized by the presence of Nutriose®, which was located in both the inter-lamellar and inter-v…

Male0301 basic medicineBiodistributionAntioxidantCurcuminEstrès oxidatiumedicine.medical_treatmentPhospholipidBiological AvailabilityCurcumin analogues02 engineering and technologyAntioxidants03 medical and health scienceschemistry.chemical_compoundCryoprotective AgentsDrug Delivery SystemsCurcumaMicroscopy Electron TransmissionX-Ray DiffractionDextrinsScattering Small AnglemedicineZeta potentialAnimalsHumansTissue DistributionGeneral Materials ScienceRats WistarPhospholipidsInflammationchemistry.chemical_classificationVesicle021001 nanoscience & nanotechnologyRats3. Good healthBioavailabilityIntestinesOxidative StressFreeze DryingPrebiotics030104 developmental biologychemistryCurcuminBiophysicsDextrinCaco-2 Cells0210 nano-technology
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Mangiferin glycethosomes as a new potential adjuvant for the treatment of psoriasis

2020

[EN] Mangiferin, a natural compound isolated from Mangifera indica L, was incorporated in glycerosomes, ethosomes and alternatively in glycerol-ethanol phospholipid vesicles (glycethosomes). Actually, only glycethosomes were able to stably incorporate the mangiferin that was loaded at increasing concentrations (2, 4, 6, 8 mg/mL). The morphology, size distribution, rheological properties, surface charge and entrapment efficiency of prepared vesicles were deeply measured. All vesicles were mainly spherical, oligolamellar, small in size (similar to 145 nm) and negatively charged (similar to-40 mV), as confirmed by cryo-TEM observation and dynamic laser light scattering measurements. The higher…

GlycerolAntioxidantDrug CompoundingXanthonesmedicine.medical_treatmentPharmaceutical Science02 engineering and technologyAdministration Cutaneous030226 pharmacology & pharmacyMice03 medical and health scienceschemistry.chemical_compound0302 clinical medicineIn vivoPhospholipid vesiclesGlycerolmedicineAnimalsHumansPsoriasisTissue DistributionMangiferinHydrogen peroxidePhospholipidsSkin permeationAdjuvants PharmaceuticDrug CarriersWound HealingMangiferaEthanolVesicle3T3 CellsHydrogen Peroxide021001 nanoscience & nanotechnologyIn vitroDisease Models AnimalchemistryBiophysicsMangiferinGlycethosomesTetradecanoylphorbol AcetateFemaleAntioxidantEpidermis0210 nano-technologyDrug carrierInternational Journal of Pharmaceutics
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Enhancement of nortriptyline penetration through human epidermis: influence of chemical enhancers and iontophoresis.

2008

Abstract Different known percutaneous chemical enhancers and iontophoresis have been tested in-vitro to study their ability to increase transdermal absorption of nortriptyline hydrochloride (20 mg mL−1). The chemicals 1-dodecanol, Span 20, Azone, (R)-(+)-limonene or isopropyl myristate were used as an overnight pretreatment at 5% (w/w) in ethanol. Furthermore, isopropyl myristate (20%, w/w) and propylene glycol (15%, w/w) were tested in the same vehicle. Iontophoresis was applied directly to the nortriptyline hydrochloride donor solution for three different concentrations (20, 2 and 0.5 mgmL−1). The chemical enhancers slightly increased the nortriptyline transdermal flux but iontophoresis w…

AdultSkin AbsorptionPharmaceutical ScienceNortriptylinePharmacologyAntidepressive Agents TricyclicIn Vitro TechniquesAdministration CutaneousPermeabilityDiffusionchemistry.chemical_compoundCyclohexenesmedicineHumansIsopropyl myristateTransdermalHexosesPharmacologyChromatographyEthanolIontophoresisMyristatesTerpenesPenetration (firestop)AzepinesIontophoresisMiddle AgedchemistryNortriptyline HydrochlorideDodecanolFemaleNortriptylineEpidermisPharmaceutical VehiclesHEPESAzoneLimonenemedicine.drugThe Journal of pharmacy and pharmacology
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Hydroxypropylmethylcellulose films for the ophthalmic delivery of diclofenac sodium

2012

Abstract Objectives The aim of this study was to prepare diclofenac/hydroxypropylmethylcellulose (HPMC) and diclofenac-loaded nanoparticles/HPMC films as potential systems for ocular delivery. Methods Two different concentration of the polymer were used: 1.5 and 2.0% w/v. Chitosan–hyaluronic acid nanoparticles were prepared by the ionotropic gelation technique. Nanoparticles were characterized by transmission electron microscopy, dynamic light scattering, drug encapsulation efficiency and rheological studies. In-vitro drug studies and corneal penetration release studies were carried out. Drug release mechanism was finally evaluated by fitting the Ritger and Peppas equation to data. In addit…

DiclofenacPolymersPharmaceutical ScienceNanoparticleAdministration OphthalmicMethylcellulosePharmacologyPermeabilityDosage formDrug Delivery SystemsHypromellose DerivativesDiclofenacDynamic light scatteringmedicineHyaluronic AcidDosage FormsPharmacologychemistry.chemical_classificationChitosanChemistryAnti-Inflammatory Agents Non-SteroidalDiclofenac SodiumPolymerPermeationHypromellose DerivativesNanoparticlesmedicine.drugNuclear chemistryJournal of Pharmacy and Pharmacology
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Fabrication of quercetin and curcumin bionanovesicles for the prevention and rapid regeneration of full-thickness skin defects on mice

2013

In the present work biocompatible quercetin and curcumin nanovesicles were developed as a novel approach to prevent and restore skin tissue defects on chronic cutaneous pathologies. Stable and suitable quercetin- and curcumin-loaded phospholipid vesicles, namely liposomes and penetration enhancer-containing vesicles (PEVs), were prepared. Vesicles were made from a highly biocompatible mixture of phospholipids and alternatively a natural polyphenol, quercetin or curcumin. Liposomes were obtained by adding water, while PEVs by adding polyethylene glycol 400 and Oramix®CG110 to the water phase. Transmission electron microscopy, cryogenic-transmission electron microscopy and small- and wide-ang…

CurcuminMaterials scienceStatic ElectricitySus scrofaBiomedical EngineeringPolyethylene glycolBiochemistryBiomaterialsMicechemistry.chemical_compoundX-Ray DiffractionScattering Small AnglePEG ratioAnimalsEdemaRegenerationParticle SizeMolecular BiologyPeroxidaseSkinMice Inbred ICRLiposomeVesicleGeneral MedicineIn vitroDisease Models AnimalchemistryBiochemistryLiposomesCurcuminBiophysicsNanoparticlesFemaleQuercetinQuercetinWound healingBiotechnologyActa Biomaterialia
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Functional response of novel bioprotective poloxamer-structured vesicles on inflamed skin

2017

[EN] Resveratrol and gallic acid, a lipophilic and a hydrophilic phenol, were co-loaded in innovative, biocompatible nanovesicles conceived for ensuring the protection of the skin from oxidative-and inflammatory-related affections. The basic vesicles, liposomes and glycerosomes, were produced by a simple, one-step method involving the dispersion of phospholipid and phenols in water or water/glycerol blend, respectively. Liposomes and glycerosomes were modified by the addition of poloxamer, a stabilizer and viscosity enhancer, thus obtaining viscous or semisolid dispersions of structured vesicles. The vesicles were spherical, unilamellar and small in size (similar to 70 nm in diameter). The …

Materials scienceCell SurvivalSwineSkin AbsorptionBiomedical EngineeringPhospholipidPharmaceutical ScienceMedicine (miscellaneous)Bioengineering02 engineering and technologyPoloxamerResveratrol010402 general chemistry01 natural sciencesCell Linechemistry.chemical_compoundMiceIn vivoGallic AcidStilbenesGlycerolAnimalsEdemaGeneral Materials SciencePhenolsSkinLiposomePhenolVesicleAnti-Inflammatory Agents Non-SteroidalSkin inflammationPoloxamerFibroblasts021001 nanoscience & nanotechnology0104 chemical sciencesOxidative StresschemistryBiochemistryResveratrolLiposomesPhospholipid vesicleBiophysicsMolecular MedicineFemale0210 nano-technology
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Freeze-dried eudragit-hyaluronan multicompartment liposomes to improve the intestinal bioavailability of curcumin.

2016

This work aimed at finding an innovative vesicle-type formulation able to improve the bioavailability of curcumin upon oral administration. To this purpose, phospholipid, Eudragit® S100 and hyaluronan sodium salt were combined to obtain eudragit-hyaluronan immobilized vesicles using an easy and environmentally-friendly method. For the first time, the two polymers were combined in a system intended for oral delivery, to enhance curcumin stability when facing the harsh environment of the gastrointestinal tract. Four different formulations were prepared, keeping constant the amount of the phospholipid and varying the eudragit-hyaluronan ratio. The freeze-drying of the samples, performed to inc…

MaleCurcuminPhospholipidPharmaceutical ScienceBiological Availability02 engineering and technology010402 general chemistry01 natural sciencesIntestinal absorptionchemistry.chemical_compoundFreeze-dryingPolymethacrylic AcidsAnimalsTissue DistributionHyaluronic AcidRats WistarLiposomeChromatographyVesicleGeneral Medicine021001 nanoscience & nanotechnology0104 chemical sciencesBioavailabilityRatsFreeze DryingchemistryIonic strengthLiposomesCurcumin0210 nano-technologyBiotechnologyEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
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Acyclovir Delivery Matrices Based on Poly(Ethylene Glycol)/Chitosan Semi-Interpenetrating Networks

2007

Abstract Chitosan matrix systems have been studied as potential vehicles for the prolonged release of acyclovir (ACV). The influence of chitosan concentration (from 0.83% to 1.67%) on viscoelastic properties of formulations with and without glyoxal was analyzed. For chitosan‐poly(ethylene glycol) 400 formulations loss modulus ( G ″) are greater than storage modulus ( G ′). This corresponds to the characteristic behavior of nonstructured systems. When glyoxal was added to the chitosan‐poly(ethylene glycol) 400 formulations, gelled matrix was obtained (i.e., G ′ is higher than G ″), except for the lowest chitosan concentration. ACV release rates for the both types of systems, with and without…

RheometryViscosityChemistry PharmaceuticalDiffusionAcyclovirPharmaceutical ScienceGlyoxalDynamic mechanical analysisElasticityViscoelasticityPolyethylene GlycolsDiffusionChitosanchemistry.chemical_compoundSolubilitychemistryDynamic modulusGlyoxalOrganic chemistryEthylene glycolDrugs Chinese HerbalNuclear chemistryJournal of Pharmaceutical Sciences
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Inhibition of skin inflammation by baicalin ultradeformable vesicles.

2016

The topical efficacy of baicalin, a natural flavonoid isolated from Scutellaria baicalensis Georgi, which has several beneficial properties, such as antioxidative, antiviral, anti-inflammatory and antiproliferative, is hindered by its poor aqueous solubility and low skin permeability. Therefore, its incorporation into appropriate phospholipid vesicles could be a useful tool to improve its local activity. To this purpose, baicalin at increasing concentrations up to saturation, was incorporated in ultradeformable vesicles, which were small in size (∼67nm), monodispersed (PI<0.19) and biocompatible, regardless of the concentration of baicalin, as confirmed by in vitro studies using fibroblasts…

AdultCell SurvivalSkin AbsorptionPharmaceutical ScienceDermatitis02 engineering and technologyPharmacologyAdministration Cutaneous03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineIn vivomedicineAnimalsHumansDexamethasoneTransdermalFlavonoidsDrug CarriersbiologyEpidermis (botany)Vesicle3T3 CellsMiddle Aged021001 nanoscience & nanotechnologybiology.organism_classificationIn vitrochemistry030220 oncology & carcinogenesisScutellaria baicalensisFemale0210 nano-technologyBaicalinmedicine.drugInternational journal of pharmaceutics
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Formulation of liposomes loading lentisk oil to ameliorate topical delivery, attenuate oxidative stress damage and improve cell migration in scratch …

2021

[EN] Pistacia lentiscus L. is a sclerophyllous shrub capable of growing under harsh climatic conditions especially in the Mediterranean Basin. Different products can be obtained from this plant, such as essential oil, mastic gum or even fixed oil. The last is well known for its flavor which is mainly exploited in the food industry. Additionally, it has been traditionally used in the treatment of skin diseases, but, at the moment, any suitable formulation for skin delivery has been formulated and its biological effects was not deeply confirmed. Given that, in the present study, the lentisk oil has been formulated in liposomes at different concentrations (10, 20, 30 mg/ml) and their physicoch…

KeratinocytesSwineAdministration Topicalmedicine.disease_causelaw.inventionchemistry.chemical_compoundMiceSkin absorptionlawCell MovementScratch assayLecithinsMaterials TestingFood scienceHydrogen peroxideWound healingScratch assayFlavorLiposomeSkin permeation studiesbiologyVesiclePellGeneral MedicineOxidantsPistaciaKeratinocytes &amp; fibroblastsPistacia lentiscusFarmacologiaKeratinocytes & fibroblastsDrug CompoundingWound healingRM1-950Cell LinemedicineOils VolatileAnimalsHumansAbsorció cutàniaParticle SizeEssential oilPharmacologyOlis essencialsPenetration (firestop)Hydrogen Peroxidebiology.organism_classificationConfocal microscopyOxidative StresschemistryEssences and essential oilsPistacia lentiscusLiposomesSkin permeation studies confocal microscopyTherapeutics. PharmacologySoybeansOxidative stress
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A mathematical approach to predicting the percutaneous absorption enhancing effect of sodium lauryl sulphate.

2003

A study has been made of the effect of sodium lauryl sulphate (SLS) at several concentrations from 0.24 to 5% (w/w) on skin permeability. Seven model drugs were selected for this study on the basis of their lipophilicity as represented by their logP(oct) values (from -0.95 to 4.2). Skin pre-treatment with aqueous solutions of SLS does not increase the permeability coefficient of the most lipophilic compounds (logP(oct)> or =3). For the other compounds assayed the increase in the permeability coefficients depends on the concentration of SLS used in the skin pre-treatment, and on the lipophilicity of the compounds tested.The correlation between the inverse of SLS efficacy as an enhancer (1/ER…

Skin AbsorptionPharmaceutical ScienceAbsorption (skin)In Vitro TechniquesAdministration CutaneousModels Biologicalchemistry.chemical_compoundSurface-Active AgentsPharmacokineticsAnimalsPharmacokineticsSodium dodecyl sulfateRats WistarMathematical ComputingAqueous solutionChromatographyintegumentary systemChemistrySodium lauryl sulphateSodium Dodecyl SulfateRatsPharmaceutical PreparationsPermeability (electromagnetism)LipophilicityFemaleAzoneAlgorithmsInternational journal of pharmaceutics
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Baicalin and berberine ultradeformable vesicles as potential adjuvant in vitiligo therapy.

2018

0.5-1% of the world's population is affected by vitiligo, a disease characterized by a gradual depigmentation of the skin. Baicalin and berberine are natural compounds with beneficial activities, such as antioxidant, anti-inflammatory and proliferative effects. These polyphenols could be useful for the treatment of vitiligo symptoms, and their efficacy can be improved by loading in suitable carriers. The aim of this work was to formulate and characterize baicalin or berberine loaded ultradeformable vesicles, and demonstrate their potential as adjuvants in the treatment of vitiligo. The vesicles were produced using a previously reported simple, scalable method. Their morphology, size distrib…

KeratinocytesBerberineSwineUltraviolet Raysmedicine.medical_treatmentDrug CompoundingSkin AbsorptionPopulationStatic ElectricityVitiligo02 engineering and technologyVitiligoPharmacology01 natural sciencesAntioxidantsPermeabilityMelaninchemistry.chemical_compoundColloid and Surface ChemistryBerberineDepigmentation0103 physical sciencesmedicineAnimalsHumansPhysical and Theoretical ChemistryeducationCell Line TransformedSkinFlavonoidsMelaninseducation.field_of_studyintegumentary system010304 chemical physicsChemistryMonophenol MonooxygenaseVesicleSurfaces and InterfacesGeneral Medicine021001 nanoscience & nanotechnologymedicine.diseaseLiposomesMelanocytesmedicine.symptom0210 nano-technologyBaicalinAdjuvantSunscreening AgentsBiotechnologyColloids and surfaces. B, Biointerfaces
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Nanodesign of new self-assembling core-shell gellan-transfersomes loading baicalin and in vivo evaluation of repair response in skin

2017

Gellan nanohydrogel and phospholipid vesicles were combined to incorporate baicalin in new self-assembling core-shell gellan-transfersomes obtained by an easy, scalable method. The vesicles were small in size (~107 nm) and monodispersed (P.I. ≤ 0.24), forming a viscous system (~24 mPa/s) as compared to transfersomes (~1.6 mPa/s), as confirmed by rheological studies. Gellan was anchored to the bilayer domains through cholesterol, and the polymer chains were distributed onto the outer surface of the bilayer, thus forming a core-shell structure, as suggested by SAXS analyses. The optimal carrier ability of core-shell gellan-transfersomes was established by the high deposition of baicalin in th…

3003SwinePharmaceutical ScienceMedicine (miscellaneous)02 engineering and technology01 natural sciencesMicechemistry.chemical_compoundDrug Delivery Systemsmaterials science (all)skin deliveryGeneral Materials ScienceSkinchemistry.chemical_classificationSkin repairSmall-angle X-ray scatteringBilayerVesicleAnti-Inflammatory Agents Non-SteroidalPolysaccharides BacterialPolymer021001 nanoscience & nanotechnologymedicine.anatomical_structureMolecular MedicineFemale0210 nano-technologytransfersomesSkin AbsorptionBiomedical EngineeringgellanBioengineeringAdministration Cutaneous010402 general chemistryIn vivo studiesDermisIn vivoSAXS analysismedicineAnimalsgellan; In vivo studies; rheological studies; SAXS analysis; skin delivery; transfersomes; bioengineering; medicine (miscellaneous); molecular medicine; biomedical engineering; materials science (all); 3003rheological studiesFlavonoidsInflammationWound Healing0104 chemical sciencesAnimals NewbornchemistryLiposomesBiophysicsNanoparticlesBaicalin
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Eco-scalable baicalin loaded vesicles developed by combining phospholipid with ethanol, glycerol, and propylene glycol to enhance skin permeation and…

2019

Abstract A new class of biocompatible and scalable phospholipid vesicles was developed, aiming at improving the efficacy of baicalin on the skin. Phosphatidylcholine and baicalin (a natural polyphenol) were hydrated in two steps with a mixture of ethanol, glycerol, and propylene glycol at different ratios, and a low amount of water (4%). Hence, water was almost completely replaced by the co-solvents, which were never used before as predominant dispersing medium of phospholipid vesicles. The vesicles appeared three-dimensionally structured, forming a network that conferred a high viscosity to the dispersions. The vesicles were unilamellar, small in size (∼100 nm), and stable during 12 months…

GlycerolBiocompatibilitySurface PropertiesSwineSkin AbsorptionPhospholipid02 engineering and technology01 natural scienceschemistry.chemical_compoundColloid and Surface ChemistryPhosphatidylcholine0103 physical sciencesGlycerolAnimalsPhysical and Theoretical ChemistryParticle SizePhospholipidsTransdermalSkinFlavonoidsChromatography010304 chemical physicsEthanolVesicleSurfaces and InterfacesGeneral MedicinePermeation021001 nanoscience & nanotechnologyPropylene GlycolOxidative Stresschemistry0210 nano-technologyBaicalinBiotechnologyColloids and surfaces. B, Biointerfaces
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Topical anti-inflammatory potential of quercetin in lipid-based nanosystems: In vivo and in vitro evaluation

2013

Purpose: To develop quercetin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), and to investigate their efficacy on TPA-induced skin inflammation. Methods: Vesicles were made from a mixture of phospholipids, quercetin and polyethylene glycol 400 (PEG), specifically added to increase drug solubility and penetration through the skin. Vesicle morphology and self-assembly were probed by Cryo-Transmission Electron Microscopy and Small/Wide Angle X-ray Scattering, as well as the main physico-chemical features by Light Scattering. The anti-inflammatory efficacy of quercetin nanovesicles was assessed in vivo on TPA-treated mice dorsal skin by the d…

dermal fibroblastsmiceSkin AbsorptionAnti-Inflammatory AgentsDrug Evaluation PreclinicalPharmaceutical ScienceInflammationPharmacologyAdministration Cutaneousquercetinchemistry.chemical_compoundX-Ray DiffractionIn vivoskin inflammationmedicineAnimalsheterocyclic compoundsPharmacology (medical)PharmacologyDrug CarriersLiposomevesiclesintegumentary systemVesiclefungiOrganic Chemistry3T3 CellsPenetration (firestop)In vitrochemistryLiposomesNanoparticlesMolecular MedicineFemaleTopical anti-inflammatorymedicine.symptomQuercetinBiotechnology
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Mangiferin nanoemulsions in treatment of inflammatory disorders and skin regeneration

2018

Abstract In this paper mangiferin nanoemulsions were developed using hyaluronic acid of different molecular weight, in absence or presence of Transcutol-P. An extensive study was carried out on the physico-chemical properties of nanoemulsions. Nanosizer and transmission electron microscopy showed oil droplets average size 296 nm with monodisperses distribution (PI ≤ 0.30). The zeta potential was highly negative (−30 mV). FTIR analysis confirms the existence of physical interactions among compounds. Rheological measurements allowed to conclude that all formulations present a pseudoplastic behavior (s ∼ 0.4) in presence of the biopolymer. Moreover, mangiferin release depends on the molecular …

XanthonesAnti-Inflammatory AgentsPharmaceutical Scienceengineering.materialMicechemistry.chemical_compoundSkin Physiological PhenomenaHyaluronic acidZeta potentialAnimalsRegenerationDistribution (pharmacology)Mangiferinchemistry.chemical_classificationWound HealingChromatographyPolymerPermeationDrug LiberationchemistryPermeability (electromagnetism)engineeringNanoparticlesEmulsionsFemaleBiopolymerRheologyInternational Journal of Pharmaceutics
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Chitosomes as drug delivery systems for C-phycocyanin: preparation and characterization.

2010

The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH-XG-microcomplexes were prepared in aqueous lactic acid at different chitosan-xanthan gum percent ratios and rheological properties of the microcomplexes were studied to analyse the contribution of chitosan and xanthan gum in the reaction of microcomplexation. After establishing the best microcomplexes, chitosomes were prepared by coating C-phycocyanin loaded liposomes with the CH-XG hydrogels using spray-drying or freeze-drying. The chitos…

Surface PropertiesDrug CompoundingPharmaceutical Sciencemacromolecular substancesPharmacologyIn Vitro TechniquesModels BiologicalChitosanchemistry.chemical_compoundDrug Delivery SystemsZeta potentialmedicineAnimalsIntestinal MucosaParticle SizeRats WistarActive ingredientLiposomeChitosanPolysaccharides BacterialPhycocyaninHydrogelsElasticityRatschemistryChemical engineeringSolubilityDelayed-Action PreparationsDrug deliverySelf-healing hydrogelsLiposomesMicroscopy Electron ScanningSwellingmedicine.symptomRheologyXanthan gummedicine.drugTabletsInternational journal of pharmaceutics
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Co-Loading of Ascorbic Acid and Tocopherol in Eudragit-Nutriosomes to Counteract Intestinal Oxidative Stress

2019

The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit&reg

3003AntioxidantVitamina CVitamina Emedicine.medical_treatmentNeuroimmunologyPhospholipidPharmaceutical Sciencelcsh:RS1-441CicatritzacióWound healingNutriose02 engineering and technologymedicine.disease_causeEudragitArticlelcsh:Pharmacy and materia medica03 medical and health scienceschemistry.chemical_compoundOral administrationmedicinePhospholipid vesiclesVitamin ETocopherolVitamin C030304 developmental biology0303 health sciencesIntestinsChromatographyVesiclePrebiotic021001 nanoscience & nanotechnologyAscorbic acidIntestinal wound healingNeuroimmunologiaIntestineschemistryAntioxidant; Eudragit; Intestinal wound healing; Nutriose; Phospholipid vesicles; 3003Antioxidant0210 nano-technologyOxidative stress
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N-Succinyl-chitosan systems for 5-aminosalicylic acid colon delivery: In vivo study with TNBS-induced colitis model in rats

2011

5-Aminosalicylic acid (5-ASA) loaded N-Succinyl-chitosan (SucCH) microparticle and freeze-dried system were prepared as potential delivery systems to the colon. Physicochemical characterization and in vitro release and swelling studies were previously assessed and showed that the two formulations appeared to be good candidates to deliver the drug to the colon. In this work the effectiveness of these two systems in the treatment of inflammatory bowel disease was evaluated. In vitro mucoadhesive studies showed excellent mucoadhesive properties of both the systems to the inflamed colonic mucosa. Experimental colitis was induced by rectal instillation of 2,4,6-trinitrobenzene sulfonic acid (TNB…

Malemedicine.medical_specialtyAminosalicylic acidColonPolymersPharmaceutical ScienceLymphocyte ActivationInflammatory bowel diseaseGastroenterologyAbsorptionChitosanchemistry.chemical_compoundDrug Delivery SystemsIn vivoInternal medicinemedicineAnimalsIntestinal MucosaRats WistarMicroparticleColitisMesalaminePeroxidaseChitosanDrug CarriersChemistryAnti-Inflammatory Agents Non-SteroidalOrgan SizeColitismedicine.diseasedigestive system diseasesIn vitroRatsDisease Models AnimalFreeze DryingTrinitrobenzenesulfonic AcidSwellingmedicine.symptomInternational Journal of Pharmaceutics
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Design, characterization and in vitro evaluation of 5-aminosalicylic acid loaded N-succinyl-chitosan microparticles for colon specific delivery

2011

The objective of this study was to prepare NS-chitosan microparticles for the delivery of 5-aminosalicylic acid (5-ASA) to the colon. Microparticles can spread out over a large area of colon allowing a more effective local efficacy of 5-ASA. N-Succinyl-chitosan was chosen as carrier system because of its excellent pharmaceutical properties in colon drug targeting such as poor solubility in acid environment, biocompatibility, mucoadhesive properties, and low toxicity. It was prepared by introducing succinic group into chitosan N-terminals of the glucosamine units. 5-ASA loaded NS-chitosan microparticles were prepared using spray-drying. As a control, a matrix obtained by freeze-drying techni…

BiocompatibilityCarrier systemColonStatic ElectricityBiocompatible MaterialsNanotechnologyChitosanchemistry.chemical_compoundDrug Delivery SystemsColloid and Surface ChemistryDifferential scanning calorimetryX-Ray DiffractionSpectroscopy Fourier Transform InfraredmedicineZeta potentialHumansDesiccationParticle SizePhysical and Theoretical ChemistrySolubilityMesalamineChitosanCalorimetry Differential ScanningSurfaces and InterfacesGeneral MedicineHydrogen-Ion ConcentrationMicrospheresKineticsFreeze DryingSolubilitychemistryTargeted drug deliveryMicroscopy Electron ScanningWettabilitySwellingmedicine.symptomRheologyBiotechnologyNuclear chemistryColloids and Surfaces B: Biointerfaces
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Skin permeation model of phenyl alcohols: comparison of experimental conditions

1998

Abstract This study was conducted primarily to establish the significance of the experimental conditions in the determination of permeability coefficients. In order to do this, standard in vitro skin permeation methods were used to determine the permeability coefficient (kp) of a homologous series of phenyl alcohols, with a wide range of lipophilicity, by two different experimental conditions through rat skin; first, using solutions (at 75% saturation concentration) of the penetrants in the donor compartment and second using saturated solutions added with an excess of the penetrant. The kp values obtained by these techniques were compared. Solubility of the phenyl alcohols in the donor phas…

Partition coefficientHomologous serieschemistry.chemical_compoundChromatographyPenetrant (mechanical electrical or structural)chemistryBenzyl alcoholLipophilicityPharmaceutical SciencePhysical chemistrySolubilityPermeationSaturation (chemistry)International Journal of Pharmaceutics
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Alternative Methods to Animal Testing in Safety Evaluation of Cosmetic Products

2018

Abstract This chapter reviews alternative methods recommended for animal testing in various toxicological areas. An alternative model to achieve complete animal replacement for acute toxicity testing is not possible. Skin corrosion/irritation alternative methods have been validated and accepted. For eye irritation testing, no single method is able to replace the Draize rabbit eye test. Skin sensitization methods imply refinement and reduction of numbers of animals. An in vitro dermal absorption test could be an alternative to in vivo testing. There are no generally accepted alternative methods to replace the usual repeated-dose toxicity in vivo assays. To determine the genotoxic and mutagen…

0301 basic medicineAlternative methodsbusiness.industrySkin sensitizationDevelopmental toxicityBioinformaticsmedicine.disease_cause03 medical and health sciences030104 developmental biology0302 clinical medicineToxicityMedicineIrritationAnimal testingbusinessPhototoxicityAcute toxicity testing030217 neurology & neurosurgery
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Influence of sodium lauryl sulphate on the in vitro percutaneous absorption of compounds with different lipophilicity

1997

Abstract The effects of sodium lauryl sulphate (SLS) at different concentrations on the “in vitro” percutaneous absorption of a number of compounds (5-fluorouracil, antipyrine, pentoxifylline, salicylamide, 4-ethylaniline, 4-n-butylaniline and indomethacin) with a wide range of lipophilicity values (log POCT from −0.95 to 4.42) through rat skin were analysed. After pretreatment of the skin with SLS (1% and 5%, w/w) the permeability coefficients increased only for compounds having a log POCT

Chromatographyintegumentary systemPermeability (electromagnetism)ChemistrySodium lauryl sulphateLipophilicityPercutaneous absorptionmedicinePharmaceutical ScienceSalicylamideIn vitroPentoxifyllinemedicine.drugEuropean Journal of Pharmaceutical Sciences
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Delivery of liquorice extract by liposomes and hyalurosomes to protect the skin against oxidative stress injuries.

2015

Liquorice extract, obtained by percolation in ethanol of Glycyrrhiza glabra L. roots, was incorporated in liposomes and hyalurosomes, new phospholipid-sodium hyaluronate vesicles, and their protective effect against oxidative stress skin damages was probed. As a comparison, raw glycyrrhizin was also tested. All the vesicles were small in size (≤ 100 nm), with a highly negative zeta potential ensuring long-term stability, and able to incorporate a high amount of the extract. In vitro tests showed that the liquorice extract loaded in vesicles was able to scavenge DPPH free radical (80% inhibition) and to protect 3T3 fibroblasts against H2O2-induced oxidative stress, restoring the normal condi…

AntioxidantPolymers and PlasticsDPPHmedicine.medical_treatmentAdministration TopicalChemistry PharmaceuticalPharmacologymedicine.disease_causePlant Rootschemistry.chemical_compoundMiceDrug StabilityIn vivoCell MovementMaterials TestingMaterials ChemistrymedicineGlycyrrhizaAnimalsEdemaHyaluronic AcidGlycyrrhizinCell ProliferationSkinLiposomeDrug CarriersbiologyPlant ExtractsOrganic Chemistry3T3 CellsFree Radical Scavengersbiology.organism_classificationOxidative StresschemistryBiochemistryLiposomesGlycyrrhizaFemaleDrug carrierOxidative stressCarbohydrate polymers
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Enhancing effect of alpha-hydroxyacids on "in vitro" permeation across the human skin of compounds with different lipophilicity.

2005

The percutaneous penetration-enhancing effects of glycolic acid, lactic acid and sodium lauryl sulphate through the human epidermis was investigated using 5-fluorouracil as a hydrophilic model permeant and three compounds belonging to the phenylalcohols: 2-phenyl-ethanol, 4-phenyl-butanol and 5-phenyl-pentanol. The lipophilicity values of the compounds ranged from log Poct -0.95 to 2.89. The effect of the enhancer concentration was also studied. Skin pretreatment with aqueous solutions of the three enhancers did not increase the permeability coefficient of the most lipophilic compound (log Poct = 2.89). For the other compounds assayed, the increase in the permeability coefficients depended …

AdultButanolsSkin AbsorptionPharmaceutical ScienceHuman skinIn Vitro TechniquesPermeabilitychemistry.chemical_compoundPentanolsHumansLactic AcidGlycolic acidTransdermalSkinChromatographyAqueous solutionSodium Dodecyl SulfatePermeationPhenylethyl AlcoholLactic acidGlycolateschemistryPermeability (electromagnetism)AlcoholsLipophilicityFemaleFluorouracilEpidermisHydroxy AcidsInternational journal of pharmaceutics
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Entrapment of Citrus limon var. pompia Essential Oil or Pure Citral in Liposomes Tailored as Mouthwash for the Treatment of Oral Cavity Diseases

2020

This work aimed at developing a mouthwash based on liposomes loading Citrus limon var. pompia essential oil or citral to treat oropharyngeal diseases. Vesicles were prepared by dispersing phosphatidylcholine and pompia essential oil or citral at increasing amounts (12, 25 and 50 mg/mL) in water. Transparent vesicle dispersions were obtained by direct sonication avoiding the use of organic solvents. Cryogenic transmission electron microscopy (cryo-TEM) confirmed the formation of unilamellar, spherical and regularly shaped vesicles. Essential oil and citral loaded liposomes were small in size (~110 and ~100 nm, respectively) and negatively charged. Liposomes, especially those loading citral, …

0301 basic medicineLemonsSonicationkeratinocyte migrationlcsh:Medicinelcsh:RS1-441Pharmaceutical Sciencehydrogen peroxide02 engineering and technologyMalalties de la bocaCitral<i>Streptococcus mutans</i>law.inventionlcsh:Pharmacy and materia medica03 medical and health scienceschemistry.chemical_compoundlawPhosphatidylcholinescratch assayDrug DiscoveryLlimonesanticaries activityKeratinocyte migration<i>Citrus limon</i> essential oilHydrogen peroxideEssential oilLiposomeOlis essencialsChromatographyVesiclelcsh:RStreptococcusEstreptococs021001 nanoscience & nanotechnology030104 developmental biologyMouth diseaseschemistryEssences and essential oilsMolecular Medicine0210 nano-technology
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A novel ultradeformable liposomes of Naringin for anti-inflammatory therapy

2018

[EN] Ultradeformable liposomes were formulated using naringin (NA), a flavanone glycoside, at different concentrations (3, 6 and 9 mg/mL). Nanovesicles were small size (similar to 100 nm), regardless of the NA concentration used, and monodisperse (PI<0.30). All formulations showed a high entrapment efficiency (similar to 88%) and a highly negative zeta potential (around -30 mV). The selected formulations were highly biocompatible as confirmed by in vitro studies using 3T3 fibroblasts. In vitro assay showed that the amounts (%) of NA accumulated in the epidermis (similar to 10%) could explain the anti-inflammatory properties of ultradeformable liposomes. In vivo studies confirmed the higher …

0301 basic medicineAnti-Inflammatory AgentsDermatitis02 engineering and technologyPharmacologyMicechemistry.chemical_compoundColloid and Surface ChemistryZeta potentialSkinLiposomeTransdermal penetrationPellSurfaces and InterfacesGeneral Medicine021001 nanoscience & nanotechnologyFlavanonesPhosphatidylcholinesTetradecanoylphorbol AcetateBetamethasoneFemale0210 nano-technologyFlavanoneBiotechnologymedicine.drugAntiinflamatorisCell Survivalmedicine.drug_classDrug CompoundingSkin AbsorptionAdministration CutaneousIn vivo studiesAnti-inflammatory03 medical and health sciencesIn vivomedicineAnimalsPhysical and Theoretical ChemistryNaringinUltradeformable liposomesPhosphatidylethanolaminesLysophosphatidylcholinesFibroblastsIn vitro030104 developmental biologychemistryLiposomesNIH 3T3 CellsAnti-inflammatoryNaringin
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Innovative strategies to treat skin wounds with mangiferin: fabrication of transferosomes modified with glycols and mucin

2020

Aim: The moisturizing properties of glycerol, the penetration enhancing capability of propylene glycol and the bioadhesive properties of mucin were combined to improve the carrier capabilities of transfersomes and the efficacy of mangiferin in the treatment of skin lesions. Materials &amp; methods: Mangiferin was incorporated in transfersomes and glycoltransfersomes, which were also modified with mucin. The physico–chemical features were assessed, along with the efficacy against oxidative stress and skin wounds in vitro and in vivo. Results: Glycoltransfersomes promoted the deposition of mangiferin in epidermis and dermis, protected fibroblasts from oxidative stress and stimulated their pr…

BioadhesiveXanthonesBiomedical EngineeringMedicine (miscellaneous)Bioengineering02 engineering and technologyDevelopmentPharmacologymedicine.disease_cause030226 pharmacology & pharmacy03 medical and health scienceschemistry.chemical_compoundGlycols0302 clinical medicineDermisIn vivoGlycerolmedicineGeneral Materials ScienceMangiferinSkinGlicolsWound Healingintegumentary systemMucinMucins021001 nanoscience & nanotechnologySkin diseasesmedicine.anatomical_structurechemistryMalalties de la pell0210 nano-technologyWound healingOxidative stress
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Co-loading of finasteride and baicalin in phospholipid vesicles tailored for the treatment of hair disorders

2020

[EN] Hair loss affects a large number of people worldwide and it has a negative impact on the quality of life. Despite the availability of different drugs for the treatment of hair disorders, therapeutic options are still limited and scarcely effective. An innovative strategy to improve the efficacy of alopecia treatment is presented in this work. Finasteride, the only oral synthetic drug approved by Unites States Federal Drug Administration, was loaded in phospholipid vesicles. In addition, baicalin was co-loaded as an adjuvant. Their effect on hair growth was evaluatedin vitroandin vivo. Liposomes, hyalurosomes, glycerosomes and glycerol-hyalurosomes were manufactured by using a simple me…

medicine.medical_treatment02 engineering and technologyPharmacologyMice03 medical and health scienceschemistry.chemical_compound0302 clinical medicineIn vivomedicineAnimalsGeneral Materials SciencePhospholipidsFlavonoidsLiposomeintegumentary systemChemistryVesicleFinasteride021001 nanoscience & nanotechnologymedicine.diseaseMice Inbred C57BLHair loss030220 oncology & carcinogenesisHair DisorderQuality of LifeFinasteride0210 nano-technologyAdjuvantBaicalin
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Transdermal nortriptyline hydrocloride patch formulated within a chitosan matrix intended to be used for smoking cessation.

2010

The aim of this study was to prepare and characterize both physically and biopharmaceutically, a nortriptyline hydrochloride (NTP-HCl) patch formulated in chitosan.16 g of each chitosan patch formulation (I, II and III, see Table 1 ) was poured onto rectangular glass plates (64 cm²) at a height of 1 mm and dried for 24 h at room temperature. In order to characterize the chitosan patches, polarized microscopy, in vitro skin permeation studies by passive diffusion and iontophoresis and rheological and bioadhesion studies were performed.Polarized microscopy revealed the absence of aggregates and crystal forms of NTP-HCl in all transdermal patches after 30 days of storage. The rheological behav…

AdultMaterials scienceTransdermal patchPharmaceutical ScienceTransdermal PatchNortriptylinePharmacologyAntidepressive Agents TricyclicChitosanchemistry.chemical_compoundHumansTransdermalSkinPolarized light microscopyChitosanIontophoresisAdrenergic Uptake InhibitorsGeneral MedicineAdhesionPermeationIontophoresisMiddle AgedchemistryChemical engineeringNortriptyline HydrochlorideFemaleSmoking CessationPharmaceutical development and technology
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A modelistic approach showing the importance of the stagnant aqueous layers in in vitro diffusion studies, and in vitro-in vivo correlations

1991

Abstract The present study deals with the role of the aqueous diffusion layers on the in vitro penetration of xenobiotics across artificial lipoidal membranes, and their ability to reproduce biophysical absorption models when in vivo results are to be simulated from the in vitro tests. The aqueous boundary layers which are invariably formed on artificial lipoidal membranes can be optionally preserved or disrupted, according to the type of absorption site which should be simulated, a condition which could reasonably lead to a better correspondence between in vitro and in vivo results; in practice, disruption of water layers can be easily achieved by a synthetic surfactant solution at its cri…

Aqueous solutionMembranePulmonary surfactantChemical engineeringIn vivoChemistryCritical micelle concentrationSynthetic membraneAnalytical chemistryPharmaceutical ScienceBiological membranePenetration (firestop)International Journal of Pharmaceutics
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In vitro study of N-succinyl chitosan for targeted delivery of 5-aminosalicylic acid to colon

2011

In vitro study on N-succinyl chitosan and chitosan (control) matrices for selective colon delivery of 5-aminosalicylic acid is described. Matrices containing β-cyclodextrin were also prepared. As shown by DSC analyses, the drug was successfully loaded into the matrices reaching up to 95% entrapment efficiency. Swelling and drug release were studied at pH 1.2, pH 7.4, and in a pH gradient medium to simulate the gastro-intestinal transit. Main result of this study was a higher capability of N-succinyl chitosan alone to better control drug release in the simulated gastro-intestinal transit: N-succinyl chitosan gave the lowest release in acid medium (≅15%) and the highest in alkaline environmen…

Drugchemistry.chemical_classificationAminosalicylic acidPolymers and PlasticsCyclodextrinmedia_common.quotation_subjectOrganic Chemistrytechnology industry and agricultureAdhesioncarbohydrates (lipids)Chitosanchemistry.chemical_compoundchemistryPolymer chemistryMaterials ChemistryPh gradientmedicineIn vitro studySwellingmedicine.symptommedia_commonNuclear chemistryCarbohydrate Polymers
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Nanocarriers for antioxidant resveratrol: formulation approach, vesicle self-assembly and stability evaluation.

2013

In this work we studied various nanoformulations of resveratrol in phospholipid vesicles. Conventional phophatidylcholine liposomes were prepared and characterized in parallel with PEVs (Penetration Enhancer-containing Vesicles) obtained by adding one of eight selected amphiphilic penetration enhancers (PEs; 0.2% w/v; HLB range 1-16) to the composition. All vesicles were around 100 nm, negatively charged (∼-30 mV) and able to incorporate resveratrol in good yields (>74%). The structure and the lamellar self-organization of the vesicles were investigated by Transmission Electron Microscopy (TEM) and Small and Wide Angle X-ray Scattering (SWAXS). These analyses showed that the lamellarity of …

Chemical PhenomenaDPPHChemistry PharmaceuticalResveratrolAntioxidantschemistry.chemical_compoundColloidColloid and Surface ChemistryDrug StabilityMicroscopy Electron TransmissionPicratesX-Ray DiffractionAmphiphileStilbenesPhysical and Theoretical ChemistryUnilamellar LiposomesLiposomeDrug CarriersChromatographyChemistryVesicleBiphenyl CompoundsSurfaces and InterfacesGeneral MedicinePenetration (firestop)ResveratrolNanoparticlesNanocarriersBiotechnologyColloids and surfaces. B, Biointerfaces
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Rheological characterization of chitosan matrices: Influence of biopolymer concentration

2007

Viscoelastic properties of chitosan (CH), chitosan-poly(ethylene glycol) 400 (CH-PEG), and chitosan-poly(ethylene glycol) 400 with glyoxal as crosslinking agent (CH-PEG-Gly) systems were studied to analyze the effect of chitosan concentration (from 0.83 to 1.67%). Dynamic moduli increase as chitosan concentration increases for all systems. For CH and CH-PEG systems the loss modulus (G″) is greater than the storage modulus (G′) with predominance of the viscous over the elastic behavior. This corresponds to the characteristic behavior of solutions (nonstructured systems). The presence of PEG 400 induces a complementary reinforcement of the mechanical properties of the system. Except for the l…

PEG 400Materials sciencePolymers and PlasticsRheometrytechnology industry and agricultureConcentration effectmacromolecular substancesGeneral ChemistryDynamic mechanical analysisViscoelasticitySurfaces Coatings and Filmschemistry.chemical_compoundChemical engineeringchemistryDynamic modulusMaterials ChemistryGlyoxalComposite materialEthylene glycolJournal of Applied Polymer Science
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Nuevo escenario en el ámbito de los productos sanitarios en la Unión Europea: Suiza y Reino Unido se convierten en terceros países

2022

Resumen Objetivo: Comparar las medidas que se han tomado por parte de la Unión Europea, Suiza y Reino Unido para mantener la continuidad de mercado cumpliendo con los requisitos regulatorios del Reglamento 745/2017 de Productos Sanitarios. Método: Para realizar este trabajo se han revisado las webs oficiales de la Comisión Europea, la Agencia Española del Medicamento y Productos Sanitarios, la Swiss Agency for Therapeutic Products y la Medicines and Healthcare Products Regulatory Agency del Reino Unido y se han realizado búsquedas bibliográficas en PubMed y en internet (Google) con términos como &#8220;withdrawal Mutual Recognition Agreement of certificates of conformity European Union Swit…

ReglamentoIrlanda del NorteSuizaAcuerdo de Reconocimiento MutuoReino UnidoProducto sanitario
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